Abstract
Digital pills, gelatin capsules with radiofrequency transmitters activated by stomach chloride ions, directly measure antiretroviral therapy adherence. In individuals with substance use disorders and HIV, real-time nonadherence detected by digital pills creates a platform to deliver substance use and adherence interventions. In this study, we determined the bioequivalence of tenofovir (TFV), administered as tenofovir disoproxil fumarate (TDF) in healthy human volunteers administered a commercial drug product and a digital pill formulation. We adhered generally to the US FDA Analytical Procedures and Methods for Validation for Drugs and Biologics guidelines. Ten HIV-uninfected adults without reported allergy to TFV, emtricitabine, or rilpivirine were enrolled. Participants ingested a digital pill containing TDF/emtricitabine/rilpivirine. Peripheral venous blood samples were collected at 0.5, 1, 2, 4, 8, and 24 h postingestion. After a 14-day washout period, the same participants ingested Complera™. Serial venous blood samples were collected using the same protocol as the digital pill. Liquid chromatography/mass spectrometry was used to determine a maximum concentration (Cmax), area under curve from time zero to last measured concentration (AUCo-t), and area under curve from time zero to infinity (AUCoo) of TFV. Ten participants with an average age of 27 and body mass index of 25.4 successfully completed the study. Predose TFV was undetectable before the second administration of Complera confirming adequate washout period after ingestion of the digital pill. The geometric means of AUCo-t, AUCoo, and Cmax for test and reference products were within the 95% confidence intervals and, therefore, bioequivalent. TFV overencapsulated in digital pills are bioequivalent to TFV in commercial formulations.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 361-363 |
| Number of pages | 3 |
| Journal | AIDS research and human retroviruses |
| Volume | 35 |
| Issue number | 4 |
| DOIs | |
| State | Published - Apr 1 2019 |
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ASJC Scopus subject areas
- Immunology
- Virology
- Infectious Diseases
Cite this
Short Communication : Bioequivalence of Tenofovir Component of Tenofovir/Rilpivi. / Chai, Peter R.; Pereira, Luis M.; Jambaulikar, Guruprasad D.; Carrico, Adam; O'Cleirigh, Conall; Mayer, Kenneth H.; Boyer, Edward W.
In: AIDS research and human retroviruses, Vol. 35, No. 4, 01.04.2019, p. 361-363.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Short Communication
T2 - Bioequivalence of Tenofovir Component of Tenofovir/Rilpivi
AU - Chai, Peter R.
AU - Pereira, Luis M.
AU - Jambaulikar, Guruprasad D.
AU - Carrico, Adam
AU - O'Cleirigh, Conall
AU - Mayer, Kenneth H.
AU - Boyer, Edward W.
PY - 2019/4/1
Y1 - 2019/4/1
N2 - Digital pills, gelatin capsules with radiofrequency transmitters activated by stomach chloride ions, directly measure antiretroviral therapy adherence. In individuals with substance use disorders and HIV, real-time nonadherence detected by digital pills creates a platform to deliver substance use and adherence interventions. In this study, we determined the bioequivalence of tenofovir (TFV), administered as tenofovir disoproxil fumarate (TDF) in healthy human volunteers administered a commercial drug product and a digital pill formulation. We adhered generally to the US FDA Analytical Procedures and Methods for Validation for Drugs and Biologics guidelines. Ten HIV-uninfected adults without reported allergy to TFV, emtricitabine, or rilpivirine were enrolled. Participants ingested a digital pill containing TDF/emtricitabine/rilpivirine. Peripheral venous blood samples were collected at 0.5, 1, 2, 4, 8, and 24 h postingestion. After a 14-day washout period, the same participants ingested Complera™. Serial venous blood samples were collected using the same protocol as the digital pill. Liquid chromatography/mass spectrometry was used to determine a maximum concentration (Cmax), area under curve from time zero to last measured concentration (AUCo-t), and area under curve from time zero to infinity (AUCoo) of TFV. Ten participants with an average age of 27 and body mass index of 25.4 successfully completed the study. Predose TFV was undetectable before the second administration of Complera confirming adequate washout period after ingestion of the digital pill. The geometric means of AUCo-t, AUCoo, and Cmax for test and reference products were within the 95% confidence intervals and, therefore, bioequivalent. TFV overencapsulated in digital pills are bioequivalent to TFV in commercial formulations.
AB - Digital pills, gelatin capsules with radiofrequency transmitters activated by stomach chloride ions, directly measure antiretroviral therapy adherence. In individuals with substance use disorders and HIV, real-time nonadherence detected by digital pills creates a platform to deliver substance use and adherence interventions. In this study, we determined the bioequivalence of tenofovir (TFV), administered as tenofovir disoproxil fumarate (TDF) in healthy human volunteers administered a commercial drug product and a digital pill formulation. We adhered generally to the US FDA Analytical Procedures and Methods for Validation for Drugs and Biologics guidelines. Ten HIV-uninfected adults without reported allergy to TFV, emtricitabine, or rilpivirine were enrolled. Participants ingested a digital pill containing TDF/emtricitabine/rilpivirine. Peripheral venous blood samples were collected at 0.5, 1, 2, 4, 8, and 24 h postingestion. After a 14-day washout period, the same participants ingested Complera™. Serial venous blood samples were collected using the same protocol as the digital pill. Liquid chromatography/mass spectrometry was used to determine a maximum concentration (Cmax), area under curve from time zero to last measured concentration (AUCo-t), and area under curve from time zero to infinity (AUCoo) of TFV. Ten participants with an average age of 27 and body mass index of 25.4 successfully completed the study. Predose TFV was undetectable before the second administration of Complera confirming adequate washout period after ingestion of the digital pill. The geometric means of AUCo-t, AUCoo, and Cmax for test and reference products were within the 95% confidence intervals and, therefore, bioequivalent. TFV overencapsulated in digital pills are bioequivalent to TFV in commercial formulations.
UR - http://www.scopus.com/inward/record.url?scp=85063784387&partnerID=8YFLogxK
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U2 - 10.1089/aid.2018.0073
DO - 10.1089/aid.2018.0073
M3 - Article
VL - 35
SP - 361
EP - 363
JO - AIDS Research and Human Retroviruses
JF - AIDS Research and Human Retroviruses
SN - 0889-2229
IS - 4
ER -